title: Synthesis and in-vitro anti-hepatitis B virus activity of ethyl 6-bromo-8-hydroxyimidazo[1,2-a]pyridine-3-carboxylates.
abstract: A series of ethyl 6-bromo-8-hydroxyimidazo[1,2-a]pyridine-3-carboxylate derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in HepG2.2.15 cells. Nearly half of the tested compounds were proved to be highly effective in inhibiting the replication of HBV DNA with IC(50) values ranging from 1.3 to 9.1 µM. Among them, 10o and 10s were identified as the most promising compounds.
authors.affiliation: Key Laboratory of Original New Drugs Design and Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, P.R. China.
authors.forename: Dong
authors.initials: D
authors.lastname: Chen
authors.forename: Yajing
authors.initials: Y
authors.lastname: Liu
authors.forename: Shulan
authors.initials: S
authors.lastname: Zhang
authors.forename: Dexiang
authors.initials: D
authors.lastname: Guo
authors.forename: Chunhong
authors.initials: C
authors.lastname: Liu
authors.forename: Sai
authors.initials: S
authors.lastname: Li
authors.forename: Ping
authors.initials: P
authors.lastname: Gong
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002264:Carboxylic Acids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D004261:DNA Replication / Q000187:drug effects; D004279:DNA, Viral / Q000187:drug effects; D006515:Hepatitis B virus / Q000187:drug effects*; D006801:Humans; D020128:Inhibitory Concentration 50; D013329:Structure-Activity Relationship; D014779:Virus Replication / Q000187:drug effects
chemical_list: D000998:Antiviral Agents; D002264:Carboxylic Acids; D004279:DNA, Viral